ADME 1 Flashcards
Define ADME.
Factors that determine the systemic levels of a drug over time.
Absorption?
Entry of a drug into the body and is related to the route of administration.
Distribution
Refers to the range of tissues that a drug will reach.
Metabolism
Refers to the metabolic processes of the body that act on and modify the drug structure.
Elimination
Route of elimination from the body.
What is Pharmacokinetics?
How the drug concentration is affected by the body.
What is Pharmacodynamics?
This describes how the drug acts on the body.
What drug properties will effect its pharmacokinetics?
Size, hydrophobicity, charge, solubility, ability to bind to lipids and proteins and structural similarities to endogenous compound that might make it more susceptible to enzyme degradation.
Formulation of the drug and the route of delivery as well as the drugs stabilityt to the body ( pH) will also play as a factor.
Describe the process of absorption.
This is the process by which the drug moves from the site of admin to body.
How do different delivery mechs alter drug absorption properties.
Dependent of the location in which the drug is delivered the drug may need to pass through a single layer of cell or multiple layers.
For example- GI is simple but is slower since the drug must reach the are then cross over to the body supply while inhalation is very quick and is quickly absorbed into the blood.
How do hydrophilic drugs move through a membrane?
And what are the types?
These drugs require a transport mech.
These mechs include passive and active diffusion as well as endocytosis.
Similarity to endogenous compounds might enable a drug to move through
Identify routes of administration-
Subcutaneous
Intranasal
Sublingual
Buccal
Intra-dermal
Intravenous
Intra-arterial
Under the Skin
In the nasal mucosa
Under the tongue
In the cheek
Injected into the dermis of skin
Into a the vein
Into an artery
Identify routes of administration-
Intracardiac
Intramuscular
Intramammary
Intrathecal, epidural, subdural
Ocular
Retro- orbital
Directly in the heart
Into the muscle
Into the mammary gland
Into the brain, the dura or under the dura
Into the eye
Behind the eye
Identify routes of administration-
Topical
Inhalation
Rectal
Vaginal
On the skin surface
Aerosolized into the lung
Into the rectum ( suppositories)
Inside the vagina
What are the benefits of the ORAL/GI delivery?
Simple administration/ low risk of infection
Formulation can determine rate of delivery-rapid of slow release
Slow onset
Some drug can be degraded by the GI
Exposed to first pass metabolism
What are Benefits of Parenteral (subcutaneous, intramuscular and intravenous)
Fast delivery Rate is determined by location Can be delivered to specific tissues Can avoid first pass metabolism Higher risk for infection Potential adverse reaction due to rapid delivery
Identify the benefit of Mucosal delivery
Very fast
Low infection risk
Direct delivery to targets
Avoid first pass metabolism
Identify the benefits for transdermal delivery
Ease of application Higher compliance rate Consistent delivery rate over long periods Stable pharmacokinetics Works best with hydrophobic drugs Can be used for hormones and peptides
Benefits for topical delivery
Ease of application
Local site delivery
Not useful for drugs that need to enter systemic circulation
Benefits for inhalation delivery
Very fast acting
Direct access to systemic circulation
Direct access to site
Drug must be aerosolized
Drugs that are similar to Endogenous compounds move through by?
Use of a cellular carrier protein such as a transporter.
Binding to a surface receptor might facilitate what?
Endocytosis of the drug
Mechanisms that transfer across a cell membrane include?
Passive transport(diffusion), Facilitated diffusion via a concentration gradient, facilitated diffusion, active transport,pinocytosis and receptor mediated endocytosis.
A highly hydrophobic mole could be transported by?
Simple Diffusion
Molecules binding to surface receptors could be transported by?
Receptor mediated endocytosis
Molecules that bind to endogenous transporters could be transported by
Membrane transporters.
